Endothelin Receptor antagonisten (Endothelin Receptor Antagonists)

ETA Receptor which is a G-protein-coupled receptor for ETs which are three small peptides: ET-1, ET-2 and ET3. ET-1 activates various kinases that are known to be involved in the survival of cell signalling and proliferation, including protein kinase C (PKC), epidermal growth factor (EGF), insulin-like growth factor-1 and mitogen-activated protein kinase (MAPK). ETA Receptor also contributes to induction of the early-response genes c-FOS, c-JUN and c-MYC. The downstream mediators of ETA-receptor include SHC, GRB2, p38 and ERK. ET-1 acting through ETA can inhibits paclitaxel-induced apoptosis by triggering anti-apoptotic signalling through BCL2-dependent and phosphatidylinositol 3-kinase-mediated Akt pathways.